In order to target celecoxib which is a COX2 inhibitor, with potentials in the prevention and treatment of colitis and colon cancer, it was formulated as microparticles using the solvent/ evaporation method and various pH-dependent Eudragit polymers. The in-vitro evaluation of the prepared microparticles showed spherical and smooth morphology. The encapsulation efficiency and yield were high, indicating that the method used is simple and efficient at this scale. The in-vitro release study showed no release in the acidic medium for 2 h followed by the release of the drug in pH 6.8 in case of Eudragit L100-55 and L100 and pH 7.4 in case of Eudragit S100. The pharmacokinetic parameters were calculated and method validation was performed to insure that it is suitable and reliable. Pharmacokinetic parameters were investigated by determining the C max , T max , AUC 0-t , K el , and t 1/2 of the drug as a suspension and as microparticles. There was a significant difference (p50.05) in T max between the drug as a suspension and as microparticles. The effect of celecoxib on the degree of inflammation was examined on acetic acid induced colitis rat model and the drug was given as a suspension and as microparticles. The evaluation was done using macroscopical, microscopical and biochemical examination. There was a significant difference between the acetic acid control group and the treatment groups regarding all examination criteria in the order microparticles formulated using Eudragit S100 followed by Eudragit L100-55 while microparticles using Eudragit L100 and drug suspension showed almost the same results.

No abstract

No abstract

A simple, selective, rapid, sensitive and less costly green automated solid phase extraction bio-analytical high-performance liquid chromatographic-based technique with fluorescence detection (Aut-SPE-BA-HPLC-FL) for the quantification of levofloxacin in human serum samples has been developed and validated. The serum samples were loaded into the chromatographic system without prior treatment and then injected into short (20 mm × 4.6 mm, 20 µm) protein-coated (PC) µBondapak CN (µBCN) silica pre-column (PC-µBCN-pre-column). Levofloxacin was retained and pre-concentrated on the head of the PC-µBCN-pre-column, while proteins and other polar components were eliminated using phosphate buffer saline (PBS), pH 7.4, as the first mobile phase in the extraction step. Levofloxacin is then transferred to the analytical column; ZORBAX Eclipse XDB-C18 (150 mm × 46 mm, 5 µm), through the aid of a column-switching valve technique, on-throughs the elution mode using the second mobile phase containing a methanol and phosphate buffer (0.05 M, pH 5) in a ratio of 70:30 (v/v). Levofloxacin signals were detected using a fluorescence detector operated at excitation/emission wavelengths of 295/500 nm. The proposed Aut-SPE-BA-HPLC-FL methodology showed linearity over a levofloxacin concentration range of 10–10,000 ng/mL (r2 = 0.9992), with good recoveries ranging from 87.12 to 97.55%. Because of the validation qualities in terms of linearity, recovery, precision, accuracy, selectivity and robustness, the Aut-SPE-BA-HPLC-FL method has been used in some clinical trials for therapeutic drug monitoring and the pharmacokinetic study of levofloxacin in human serum.